Reference of 16097-60-2 ,Some common heterocyclic compound, 16097-60-2, molecular formula is C5H3ClF3N3, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route.
Example 21 4-(4-{[2-Amino-6-(trifluoromethyl)pyrimidin-4-yl]amino}-2-fluorobenzyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonitrile 82 mg (0.31 mmol) of 4-(4-amino-2-fluorobenzyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonitrile and 67 mg (0.34 mmol) of 4-chloro-6-trifluoromethylpyrimidine-2-amine are suspended in 3 ml of water, 1.5 ml of ethanol and 0.15 ml of 4N hydrochloric acid. The reaction mixture is heated at reflux for 2 hours. After cooling, the mixture is made alkaline using dilute aqueous sodium hydroxide solution, a little methanol is added, the mixture is extracted with ethyl acetate and the solvent is removed under reduced pressure. The residue is purified by preparative HPLC. This gives crystals. Yield: 111 mg (65% of theory) LC-MS (Method 3): Rt=2.34 min. MS (ESI pos.): m/z=428 [M+H]+. 1H-NMR (DMSO-d, 300 MHz): delta=4.41 (s, 2H), 6.35 (s, 1H), 6.90 (d, 1H), 6.96 (br. s, 2H), 7.14 (t, 1H), 7.32 (dd, 1H), 7.93 (dd, 1H), 8.29 (d, 1H), 8.46 (s, 1H), 9.77 (s, 1H), 12.86 (br. s, 1H).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,16097-60-2, its application will become more common.
Reference:
Patent; Bayer HealthCare AG; US2008/269268; (2008); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia